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TPA023

Chemical Structure : TPA023

CAS No.: 252977-51-8

TPA023 (MK-0777, MK0777, TPA-023)

Catalog No.: PC-62769Not For Human Use, Lab Use Only.

TPA023 is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    TPA023 (MK-0777) is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors.
    TPA023 (MK-0777) shows much lower (50- to 2000-fold) affinities for α4 and α6 subtypes (Ki= 60 and 418 nM, respectively).
    TPA023 (MK-0777) demonstrates anxiolytic-like efficacy and anticonvulsant activity in mouse pentylenetetrazole seizure model.

    Physicochemical Properties

    M.Wt 395.442
    Formula C20H22FN7O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine

    References

    1. Atack JR, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):17-25.

    2. de Haas SL, et al. J Psychopharmacol. 2007 Jun;21(4):374-83.

    3. Carling RW, et al. J Med Chem. 2005 Nov 17;48(23):7089-92.

    4. Atack JR, et al. J Pharmacol Exp Ther. 2006 Jan;316(1):410-22.

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